Abstract:: Cancer is the deadliest disease worldwide and the development of safer chemical entities to treat cancer is one of the major challenges of medicinal chemistry. Emergence of new cases every year and development of multiple drug resistance against available molecular entities has turned the focus of researchers towards natural products. Chalcones are pharmacologically active compounds, present in plants, which have been derivatized and screened by many researchers for the treatment of cancer. Chalcones, consist of 1,3-diaryl-2-propen-1-one, is one such class exhibiting broad anticancer activities against various cancerous cell lines. The objective of this review article is to analyze the antitumor activity of the reported chalcones via distinct mechanisms adopted by these molecules underlying their inhibitory activity. The primary focus of this review is to bring the attention of researchers towards latest and important chalcones and their derivatives having potent anticancer activity adding their possible action of mechanisms against cancerous cell lines The recent literature was surveyed and it was found that chalcone analogs with electron donating groups, indolyl, quinolone, pyrazol-ol, hydroxyaminobenzamide, hydroxamic acid and pyridyl- indole groups have shown promise as potential anticancer agents following various mechanisms. Most chalcones were found to induce significant cell cycle arrest at G2/M phase hence leading to apoptosis. A number of synthetic chalcones exhibited higher efficacy due to their ability of potent tubulin polymerization as well as dynamic enzyme inhibitory activity. This review is an immense compilation of research regarding the mechanism of action of chalcones and their identification as a promising anticancer agent for future drug developments. Thus, this review article would pave way and provide ample opportunities to design future generation of novel, highly efficacious anticancer molecules with minimal toxicity.

Various functions of gold nanoparticles in conjugation with nucleic acids.

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Chalcones possess various biological properties, for example, antimicrobial, anti-inflammatory, analgesic, antimalarial, anticancer, antiprotozoal and antitubercular activity. In this study, naphthylchalcone derivatives were synthesized and characterized using H NMR C NMR, Fourier transform infrared and mass techniques. Yields for all derivatives were found to be >90%. Protein-drug interactions influence the absorption, distribution, metabolism and excretion (ADME) properties of a drug. Therefore, to establish whether the synthesized naphthylchalcone derivatives can be used as drugs, their binding interaction toward a serum protein (bovine serum albumin) was investigated using fluorescence, circular dichroism and molecular docking techniques under physiological conditions. Fluorescence quenching of the protein in the presence of naphthylchalcone derivatives, and other derived parameters such as association constants, number of binding sites and static quenching involving confirmed non-covalent binding interactions in the protein-ligand complex were observed. Circular dichroism clearly showed changes in the secondary structure of the protein in the presence of naphthylchalcones, indicating binding between the derivatives and the serum protein. Molecular modelling further confirmed the binding mode of naphthylchalcone derivatives in bovine serum albumin. A site-specific molecular docking study of naphthylchalcone derivatives with serum albumin showed that binding took place primarily in the aromatic low helix and then in subdomain II. The dominance of hydrophobic, hydrophilic and hydrogen bonding was clearly visible and was responsible for stabilization of the complex.

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